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Weight-loss drug orlistat (Xenical and Alli), even at low levels, inhibits a major detoxification enzyme (carboxylesterase-2) in the liver, kidney and gastrointestinal track, which may lead to “severe toxicity of internal organs such as the liver and kidney”

Orlistat may also alter the efficacy of certain drugs, including cancer drugs, and may increase your risk of bleeding if you take aspirin

Despite the known risks of liver damage, and other health effects, from weight loss drugs already on the market, the FDA approved two new weight loss drugs in 2012, each with its own set of significant health concerns

If you need to lose weight, switching from a carb-based diet to a fat- and protein-based diet will help rebalance your body's chemistry, and a natural side benefit of this is weight loss, and/or improved weight management once you're at an ideal weight

Orlistat: This Popular Weight Loss Drug May Cause Permanent Liver and Kidney Damage

December 26, 2012|107,601views

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By Dr. Mercola

The weight loss drug orlistat (known as Xenical by prescription and Alli, available over-the-counter) is one of the most popular on the market.

Alli is even known to flaunt the fact that it's approved by the U.S. Food and Drug Administration (FDA) in its advertisements, using such slogans as "lose weight the FDA approved way," which, to most people, makes it sound as though it's safe...

The drug, which works by inhibiting fat absorption in your intestines, has faced problems in the past, not the least of which include cramping, gas, diarrhea, anal leakage and oily underwear stains as the result of the drug's fat-blocking mechanism of action.

Now, a University of Rhode Island researcher uncovered a far more detrimental side effect, which is so severe it prompted him to immediately alert the FDA about his findings...

Xenical and Alli May Cause "Severe Toxicity of Internal Organs"

Orlistat was first approved in 1999 as a prescription weight loss drug, and later, in 2007, became approved for over-the-counter use. Because orlistat works in your intestines, it was thought that the drug mostly stayed in the intestines and was not absorbed by the body. This was not what was found by Professor Bingfang Yan, who conducted the study.

"Since it has been available over–the-counter, there has been a drastic increase of toxicity among patients using the drug. It has been linked to severe liver failure, acute pancreatic failure and acute renal (kidney) failure."

His research, indeed, showed that orlistat, even at low levels, inhibits a major detoxification enzyme (carboxylesterase-2) in the liver, kidney and gastrointestinal track. When this occurs, it may lead to "severe toxicity of internal organs such as the liver and kidney." The enzyme also plays a role in metabolizing a variety of medications, and as such orlistat may also alter the efficacy of certain drugs. In particular, the study found orlistat may:

Amplify the anti-clotting effects of aspirin, which may increase your risk of internal and external bleeding

In 2010, the FDA required Xenical and Alli to include a warning on their labels about cases of severe liver injury that had been reported with the use of the drugs, although at the time it called the side effects "rare."3

Weight Loss Drugs Have a Troubled Past

Obesity carries with it serious health risks, including cancer, heart disease and type 2 diabetes, and with rates increasing steadily it is a condition that needs to be taken seriously. However, potentially risking your life with dangerous weight loss drugs is a risk that is just too steep to take.

The serious side effects tied to Xenical and Alli are only the latest to emerge. In 2010, the weight loss drug Meridia (sibutramine) was taken off the market after studies showed it increased the risk of heart attack and stroke. The saddest part about the story is that Meridia showed signs of dangerous side effects ever since it was first approved in 1997, but was only taken off the market more than a decade later, after millions of people had already taken the drug.

In fact, when Meridia was approved it carried a warning on its label stating that the drug should not be used in people with a history of heart disease, heart failure, heart-rhythm problems or stroke. The drug, which worked by suppressing your appetite by altering levels of the brain chemicals serotonin and norepinephrine, was also widely known to raise blood pressure and heart rate, and an FDA advisory panel actually recommended against its approval in 1996 for this very reason.

Public Citizen later petitioned the FDA to ban the drug in 2002, alleging that it was responsible for causing dozens of deaths and hundreds of adverse patient reactions since it came to market. In 2005, the FDA again considered placing stricter warnings on the drug, and in January 2010 finally asked Abbott, the drug's maker, to strengthen the warning following review of preliminary data from the SCOUT study.4

The SCOUT study, which ultimately led the FDA to request the drug be removed from the market entirely, found a 28 percent increased risk of heart attack and a 36 percent increased risk of stroke in patients taking Meridia compared to placebo.

Those are steep risks for a drug that only lead to an average weight loss of 9.5 pounds a year -- hardly worth risking a fatal heart attack or stroke over. And this is quite typical for weight loss drugs, which generally only amount to a weight loss of anywhere from four to 22 pounds... 5

Why is the FDA Speeding Approval of More Weight Loss Drugs?

Despite the known risks of liver damage, and other health effects, from weight loss drugs already on the market, the FDA is moving full speed ahead to approve new options. In fiscal year 2012, the FDA approved 35 new drugs, the same number as were approved in fiscal year 2011, which they said was "among the highest number of approvals in the past decade, surpassed only by 2009 (37)."6,7 This included two new weight loss drugs – the first to hit the market since 2009:

Qsymia

A combination of two FDA-approved drugs, phentermine (the "phen" of diet drug fen-phen, which was pulled from the market in 1997 after it was linked to serious heart valve damage) and topiramate, an anti-seizure epilepsy drug. After one year of treatment with the recommended and highest daily dose of the drug, patients had an average weight loss of 6.7 percent and 8.9 percent, respectively. Along with an increased risk of birth defects (such that women must have a negative pregnancy test prior to starting on the drug), Qsymia can increase heart rate and must not be used in patients with glaucoma or hyperthyroidism.

"...This drug's effect on heart rate in patients at high risk for heart attack or stroke is not known. Therefore, the use of Qsymia in patients with recent (within the last six months) or unstable heart disease or stroke is not recommended. Regular monitoring of heart rate is recommended for all patients taking Qsymia, especially when starting Qsymia or increasing the dose."

Belviq

Belviq works by activating the serotonin 2C receptor in your brain, which may help you eat less or feel full after eating smaller amounts of food. Fen-Phen's damaging effect on the heart valve was thought to be related to activation of the serotonin 2B receptor on heart tissue, and while the FDA notes that Belviq "does not appear to activate the 2B receptor" when used at the approved dose, they are already aware of serious side effects.

"Belviq should not be used during pregnancy. Treatment with Belviq may cause serious side effects, including serotonin syndrome, particularly when taken with certain medicines that increase serotonin levels or activate serotonin receptors. These include, but are not limited to, drugs commonly used to treat depression and migraine. Belviq may also cause disturbances in attention or memory.

… Because preliminary data suggest that the number of serotonin 2B receptors may be increased in patients with congestive heart failure, Belviq should be used with caution in patients with this condition. Belviq has not been studied in patients with serious valvular heart disease. The drug's manufacturer will be required to conduct six postmarketing studies, including a long-term cardiovascular outcomes trial to assess the effect of Belviq on the risk for major adverse cardiac events such as heart attack and stroke."

In other words, although the drug is already approved, it still has to undergo extensive testing to make sure cardiovascular problems can be ruled out... and as for the weight loss "benefit," patients lost, on average, just 3 percent to 3.7 percent of their body weight after one year. While regular echocardiograms were not recommended by the FDA for people taking Belviq, Dr. Eric Felner, who was a member of the FDA advisory panel that approved the drug, told Slate.com that in his opinion:10

"If you're going to put your patient on this medication, you need to see them somewhere along the lines of every two to three months and probably get an echocardiogram at least two or three times a year."

Tips for Losing Weight Naturally: More Fat, Fewer Carbs...

Switching from a carb-based diet to a fat- and protein-based diet will help rebalance your body's chemistry, and a natural side effect of this is weight loss, and/or improved weight management once you're at an ideal weight. One explanation for this is that you don't really get fat from eating too much and exercising too little. Nor do you get fat from eating fat.

It is also vital to select healthy fats. Avoid virtually all vegetable oils that are loaded with omega-6 fats. Fried foods are also taboo. You will want to replace the lost carb calories with healthy fats like coconut oil, olives, olive oil, avocados, eggs, butter and high-fat nuts like macadamia nuts.

One researcher that has clearly established this is Dr. Richard Johnson, whose latest book, The Fat Switch, dispels many of the most pervasive myths relating to diet and obesity.

Dr. Johnson discovered the method that animals use to gain fat prior to times of food scarcity, which turned out to be a powerful adaptive benefit. His research showed that fructose activates a key enzyme, fructokinase, which in turn activates another enzyme that causes cells to accumulate fat. When this enzyme is blocked, fat cannot be stored in the cell. Interestingly, this is the exact same "switch" animals use to fatten up in the fall and to burn fat during the winter.

Fructose is the dietary ingredient that turns on this "switch," causing cells to accumulate fat, both in animals and in humans.

In essence, overeating and excess weight could be viewed as a symptom of an improper diet. It's not necessarily the result of eating too many calories, per se, but rather getting your calories from the wrong sources. In the blossoming new field of nutrigenomics, the study of how nutrients interact with your genes, food contains information, as well as nutrients and calories. That information can turn on or off the expression of certain genes, epigenetically, as it were. In simple terms, when you consume too many sugars and carbs, you set off a cascade of chemical and epigenetic reactions in your body that reprograms your level of hunger and craving for sweets:

First, fructose is metabolized differently from glucose, with the majority being turned directly intofat because fructose stimulates a powerful gene-mediated "fat switch."

Dietary carbohydrates, especially fructose, are also the primary source of a substance called glycerol-3-phosphate (g-3-p), which causes fat to become fixed in fat tissue

At the same time, high carb intake raises your insulin levels, which prevents fat from being released

Fructose further tricks your body into gaining weight by turning off your body's appetite-control system. Fructose does not suppress ghrelin (the "hunger hormone") and doesn't stimulate leptin (the "satiety hormone"), which together result in feeling hungry all the time, even though you've eaten. As a result, you overeat and develop insulin resistance, which is not only an underlying factor of type 2 diabetes, heart disease, and a long list of other chronic diseases

The resulting equation is simple: fructose and dietary carbohydrates (grains, which break down into sugar) lead to excess body fat, obesity and related health issues. Furthermore, no amount of exercise can compensate for this damage because if you eat excessive "carbs," i.e. fructose and grains — the primary ingredients NOT found in our ancestral diet — it will activate programming to cause your body to become, and remain, fat.

A reasonable goal will be to have as much as 50-70 percent of your diet as healthy fat, which will radically reduce your carbohydrate intake. It can be helpful to remember that fat is far more satiating than carbs, so if you have cut down on carbs and feel ravenous, this is a sign that you have not replaced them with sufficient amounts of healthy fat. Sources of healthy fats that you'll want to add to your diet include:

Most people will likely notice massive improvement in their health by following this approach, as they are presently consuming FAR more grain and bean carbohydrates in their diet, and any reduction will be a step in the right direction. To help you get started on the right track, review my Nutrition Plan, which guides you through these dietary changes one step at a time.

Disclaimer: The entire contents of this website are based upon the opinions of Dr. Mercola, unless otherwise noted. Individual articles are based upon the opinions of the respective author, who retains copyright as marked. The information on this website is not intended to replace a one-on-one relationship with a qualified health care professional and is not intended as medical advice. It is intended as a sharing of knowledge and information from the research and experience of Dr. Mercola and his community. Dr. Mercola encourages you to make your own health care decisions based upon your research and in partnership with a qualified health care professional. If you are pregnant, nursing, taking medication, or have a medical condition, consult your health care professional before using products based on this content.

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